Specific chemical modification of bacterial type I dehydroquinase - opportunities for drug discovery.

Type I dehydroquinase (DHQ1) is a class I aldolase enzyme that catalyzes the reversible dehydration of 3-dehydroquinic acid to form 3-dehydroshikimic acid by multistep mechanism that involves the formation of Schiff-base species. DHQ1 is present in plants and several bacterial sources but it does not have any counterpart in human cells. It has been suggested that DHQ1 may act as a virulence factor in vivo and therefore a promising target in the search for new antivirulence agents to combat widespread antibiotic resistance. This review covers recent progress in the structure-based design and chemical modifications caused by selective irreversible inhibitors. Computational studies aimed at understanding the experimentally obtained covalent modifications and inhibitory potencies of these inhibitors are also described.
AuthorsConcepción González-Bello
JournalFuture medicinal chemistry (Future Med Chem) Vol. 7 Issue 17 Pg. 2371-83 (Nov 2015) ISSN: 1756-8927 [Electronic] England
PMID26599605 (Publication Type: Journal Article)

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